HUMAN RECOMBINANT Κ OPIOID RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human OPRK1 cDNA (GenBank Accession Number NM_000912.3) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS, 10 μg/mL puromycin
Stable after minimum two months continuous growth
Background: κ Opioid Receptor (KOR) is a receptor for dynorphins. KOR inhibits neurotransmitter release by reducing calcium currents and increasing potassium conductance and may play a role in arousal and regulation of autonomic and neuroendocrine functions. Some studies suggest that stimulation of KOR improves memory dysfunctions resulting from the blockade of muscarinic M1 receptors. In addition, KOR agonists attenuate several behavioral responses induced by drugs of abuse, raising the possibility that KOR agonists may be useful for the treatment of dependence on drugs of abuse.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Ukai et al. (1995) Kappa-Opioid receptor agonists improve pirenzepine-induced disturbance of spontaneous alternation performance in the mouse. Eur J Pharmacol 281:173-178.
Hasebe et al. (2004) Possible pharmacotherapy of the opioid kappa receptor agonist for drug dependence. Ann N Y Acad Sci 1025:404-413.